BIG NEWS: deuterated #GS441524 tri-iBu ester (#VV116) is in clinical trials in Uzbekistan for #COVID19. Trials in China ๐Ÿ”œ. Developed by the one and only *Wuhan Institute of Virology*. Deuterium was added to bypass @GileadSciences ๐Ÿ’Š 1/4
@ncats_nih_gov
shine.cn/news/nation/21โ€ฆ Image
Official article published in @cell_res in September 2021 by the folk at Wuhan Institute of Virology. Original @biorxivpreprint was published in November 2020. 2/4
nature.com/articles/s4142โ€ฆ
Chinese patent by the WIV first filed in Sept 2020. WO patent filed in April 2021. Gilead's 2009 patent on 524 and the 2016 patent on #remdesivir do not include any of the compounds described in the WIV patent. Does Gilead actually own any of these WIV compounds?? 3/4 ImageImage
And there we have it. I think it's very unlikely that WIV will try and develop in the US even though they are technically not stepping on @GileadSciences' toes. We shall see...4/4 ImageImage
Accidentally posted wrong compound in the patent! The correct one is labeled A151 ( = VV116) on page 53/74 in the Chinese patent. Image

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More from @victoriacyanide

Apr 9, 2021
First-in-Woman Safety, Tolerability, and Pharmacokinetics of Orally Administered #GS441524: A Broad-Spectrum Antiviral Treatment for #COVID19. A ๐Ÿงต1/7 osf.io/am5s8/
Part 1 of the study: 750 mg GS-441524 was orally administered as a solution QD for 7 days. D1-5 were performed in the fasted state. D6-7 in the fed state. There was a slight food effect that seemed to hamper drug absorption. Cmax ~2.4-3 uM. AUC ~26-33 uM. 2/7
No AEs or lab abnormalities were observed in Part 1 of the study. Blood chemistry was normal. 3/7
Read 7 tweets
May 14, 2020
Fun fact: #remdesivir is almost certainly not the species that reaches #COVID19 patients' lungs! Its nucleoside #GS441524 is. Wrote this piece for @statnews explaining this! @GileadSciences consider aerosolizing GS-441524 prophylaxis. Pls read and RT! 1/x

bit.ly/3dIc0Au
I've been reading a lot of general audience/science articles on #remdesivir. Many of these articles seem to confuse nucleoSIDES with nucleoTIDES. Here's the difference, feat. important figures. 2/x
#remdesivir is a nucleoTIDE monophosphate analogue. #GS441524 is a nucleoSIDE analogue. 3/x
Read 10 tweets

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